AR116566A1 - Administración sostenida de polipéptidos similares a la angiopoyetina 3 - Google Patents
Administración sostenida de polipéptidos similares a la angiopoyetina 3Info
- Publication number
- AR116566A1 AR116566A1 ARP190102781A ARP190102781A AR116566A1 AR 116566 A1 AR116566 A1 AR 116566A1 AR P190102781 A ARP190102781 A AR P190102781A AR P190102781 A ARP190102781 A AR P190102781A AR 116566 A1 AR116566 A1 AR 116566A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- optionally substituted
- cycloalkyl
- drug delivery
- Prior art date
Links
- 230000002459 sustained effect Effects 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 12
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 5
- 238000012377 drug delivery Methods 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000002924 primary amino group Chemical class [H]N([H])* 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 125000005647 linker group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 1
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 abstract 1
- 101000693085 Homo sapiens Angiopoietin-related protein 3 Proteins 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 230000008878 coupling Effects 0.000 abstract 1
- 238000010168 coupling process Methods 0.000 abstract 1
- 238000005859 coupling reaction Methods 0.000 abstract 1
- 150000004292 cyclic ethers Chemical class 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000000524 functional group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 150000003335 secondary amines Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 238000013268 sustained release Methods 0.000 abstract 1
- 239000012730 sustained-release form Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/61—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/18—Growth factors; Growth regulators
- A61K38/1891—Angiogenesic factors; Angiogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/555—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
- A61K47/6903—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/475—Growth factors; Growth regulators
- C07K14/515—Angiogenesic factors; Angiogenin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Toxicology (AREA)
- Rheumatology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Neurology (AREA)
- Ophthalmology & Optometry (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
En este documento, se describen sistemas de administración de fármacos para administrar agentes biológicamente activos que comprenden aminas primarias o secundarias, o un átomo de nitrógeno de anillo de un anillo azaheteroarilo, sales farmacéuticamente aceptables de los mismos, reactivos de administración de fármacos relacionados con el mismo, composiciones farmacéuticas que comprenden los sistemas de administración de fármacos y el uso de los sistemas de administración de fármacos como terapéutica de liberación sostenida. Reivindicación 1: Un sistema de administración de fármacos o una sal farmacéuticamente aceptable del mismo que comprende D-R, que está representado por la fórmula (1), en donde D comprende un polipéptido ANGPTL3 que comprende al menos una amina primaria; y R es un enlazador adecuado para la liberación de D, donde la línea de puntos indica unión con la amina primaria; R¹ es hidrógeno o alquilo C₁₋₄; R¹ᵃ es hidrógeno o alquilo C₁₋₄, o CR¹R¹ᵃ, tomados en combinación, forman un cicloalq C₃₋₆-1,1-diílo; R² se selecciona, de modo independiente, en cada aparición, de alquilo C₁₋₄ u oxo, o dos grupos R² tomados en combinación con los átomos de carbono a los que están unidos, forman un grupo cicloalquilo C₃₋₆ fusionado o grupo espirocicloalq C₃₋₆-1,1-diílo; a es 0, 1, 2, 3 ó 4; R³ es hidrógeno o alquilo C₁₋₄; R³ᵃ es hidrógeno, alquilo C₁₋₄, o CR³R³ᵃ tomados en combinación, forman un cicloalq C₃₋₆-1,1-diílo; Y es C(O)R⁴, C(O)OR⁴, C(O)NHR⁴, C(O)NR⁵R⁶, SiR⁵R⁶R⁷, o CR¹²R¹²ᵃOR¹³; R¹² es hidrógeno o alquilo C₁₋₄; R¹²ᵃ es hidrógeno o alquilo C₁₋₄, o CR¹²R¹²ᵃ, tomados en combinación, forman un cicloalq C₃₋₆-1,1-diílo; R¹³ es alquilo C₁₋₄; o R¹² y R¹³, tomados en combinación con C(R¹²ᵃ) y O forman un éter cíclico de 5, 6 ó 7 miembros; R⁴ es alquilo C₁₋₈ o cicloalquilo C₃₋₇, en donde el cicloalquilo está opcionalmente sustituido con 0, 1, ó 2 grupos alquilo C₁₋₄ seleccionados de modo independiente y en donde el alquilo está opcionalmente sustituido con alcoxi C₁₋₄; R⁵ y R⁶ se seleccionan cada uno, de modo independiente, de alquilo C₁₋₄ y cicloalquilo C₃₋₆; R⁷ es alquilo C₁₋₈, cicloalquilo C₃₋₇, alcoxi C₁₋₈, cicloalquiloxi C₃₋₇, heterocicloalquiloxi, u -(OCHR³CH₂)ᵇO-alquilo C₁₋₄, en donde el heterocicloalquiloxi es un anillo heterocíclico saturado de 4 a 7 miembros que tiene un heteroátomo del anillo seleccionado de N, O y S y opcionalmente sustituido con 0, 1, ó 2 grupos alquilo C₁₋₄ seleccionados de modo independiente; b es un número entero de 1 a 10; Z es CH-L-A, CH-A, N-L-A, o N-A; L es un enlazador bivalente opcionalmente sustituido; A es hidrógeno, alquilo C₁₋₈, C(O)alquilo C₁₋₈, C(O)N(H)alquilo C₁₋₈, C(O)O-alquilo C₁₋₈, R¹⁰, o R¹¹, en donde el grupo alquilo está opcionalmente sustituido con 0 ó 1 R¹⁰; R¹⁰ es un grupo funcional reactivo apropiado para acoplar la fórmula (1) a un portador; y R¹¹ es un portador.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862740609P | 2018-10-03 | 2018-10-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR116566A1 true AR116566A1 (es) | 2021-05-19 |
Family
ID=68165677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190102781A AR116566A1 (es) | 2018-10-03 | 2019-10-01 | Administración sostenida de polipéptidos similares a la angiopoyetina 3 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US11389541B2 (es) |
| EP (1) | EP3860657A1 (es) |
| JP (2) | JP7336513B2 (es) |
| KR (1) | KR20210066860A (es) |
| CN (1) | CN112770782A (es) |
| AR (1) | AR116566A1 (es) |
| AU (1) | AU2019353174A1 (es) |
| BR (1) | BR112021005981A2 (es) |
| CA (1) | CA3112251A1 (es) |
| CL (1) | CL2021000819A1 (es) |
| CO (1) | CO2021004012A2 (es) |
| CR (1) | CR20210156A (es) |
| CU (1) | CU20210022A7 (es) |
| DO (1) | DOP2021000053A (es) |
| EA (1) | EA202190650A1 (es) |
| EC (1) | ECSP21022120A (es) |
| IL (1) | IL281227A (es) |
| JO (1) | JOP20210061A1 (es) |
| MX (1) | MX2021003839A (es) |
| PE (1) | PE20211646A1 (es) |
| PH (1) | PH12021550675A1 (es) |
| SG (1) | SG11202102076TA (es) |
| TW (1) | TW202027794A (es) |
| WO (1) | WO2020070675A1 (es) |
| ZA (1) | ZA202101419B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113795590B (zh) * | 2019-05-07 | 2024-11-26 | 建新公司 | 前药组合物中药物浓度的量化方法 |
| CN112220963B (zh) * | 2020-09-24 | 2022-05-24 | 哈尔滨工业大学 | 一种非溶胀uv交联壳聚糖可注射水凝胶及其合成方法 |
| TW202306970A (zh) | 2021-05-24 | 2023-02-16 | 瑞士商諾華公司 | 用於治療骨關節炎之方法 |
| EP4346876A1 (en) | 2021-05-24 | 2024-04-10 | Novartis AG | Methods for the treatment of osteoarthritis |
| JP2025531629A (ja) * | 2022-08-23 | 2025-09-24 | アステラス インスティテュート フォー リジェネレイティブ メディシン | 細胞凍結保存製剤および使用方法 |
| CN115970066B (zh) * | 2022-12-29 | 2024-09-27 | 成都爱睿康乐医疗器械有限公司 | 基于主客体相互作用的载药纳米凝胶生物润滑剂及其制备方法和应用 |
| WO2024240212A1 (zh) * | 2023-05-24 | 2024-11-28 | 云合智药(苏州)生物科技有限公司 | 用于抑制angptl3表达的rnai剂及其应用 |
| CN117379362B (zh) * | 2023-10-11 | 2024-07-19 | 首都医科大学附属北京潞河医院 | 负载血管生成素样蛋白3的水凝胶及其制备方法与应用 |
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| US5462990A (en) | 1990-10-15 | 1995-10-31 | Board Of Regents, The University Of Texas System | Multifunctional organic polymers |
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